GNE-9605

GNE-9065 is an orally bioavailable and potent inhibitor of leucine-rich repeat kinase 2 (LRRK2, IC50 = 18.7 nM). It is selective for LRRK2 over 178 kinases, inhibiting only TAK1-TAB1 >50% at a concentration of 0.1 µM. GNE-9065 (10 and 50 mg/kg) inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S mutation found in families with autosomal Parkinson's disease.Formal Name: rel-N2-[5-chloro-1-[(3R,4R)-3-fluoro-1-(3-oxetanyl)-4-piperidinyl]-1H-pyrazol-4-yl]-N4-methyl-5-(trifluoromethyl)-2,4-pyrimidinediamine. CAS Number: 1536200-31-3. Molecular Formula: C17H20ClF4N7O. Formula Weight: 449.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 20 mg/ml, Methanol: 1 mg/ml. lambdamax: 230 nm. SMILES: CNC1=C(C(F)(F)F)C=NC(NC2=C(Cl)N([C@H]3CCN(C4COC4)C[C@@H]3F)N=C2)=N1. InChi Code: InChI=1S/C17H20ClF4N7O/c1-23-15-10(17(20,21)22)4-24-16(27-15)26-12-5-25-29(14(12)18)13-2-3-28(6-11(13)19)9-7-30-8-9/h4-5,9,11,13H,2-3,6-8H2,1H3,(H2,23,24,26,27)/t11-,13-/m0/s1. InChi Key: PUXPEQJKNAWNQA-AAEUAGOBSA-N.